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Assay Detail

CHEMBL4192534

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]ifenprodil from recombinant human GluN1A/GluN2B receptor expressed in mouse L(tk-) cell membranes after 120 mins by microbeta scintillation counting method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors.
Dey S, Temme L, Schreiber JA, Schepmann D, Frehland B, Lehmkuhl K, Strutz-Seebohm N, Seebohm G, Wünsch B.
Eur J Med Chem (2017) 138 : 552 -564
PubMed 28704758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.86 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217195 1 8.66
CHEMBL4208912 1 8.22
CHEMBL305187 IFENPRODIL 2.0 1 8.00
CHEMBL28564 ELIPRODIL 2.0 1 7.89
CHEMBL4207886 1 7.80
CHEMBL4216511 1 7.17
CHEMBL4216762 1 7.12
CHEMBL4204069 1 6.96
CHEMBL4208375 1 6.96
CHEMBL4212243 1 6.89
CHEMBL4213309 1 6.68
CHEMBL4215178 1 6.64
CHEMBL4203530 1 6.62
CHEMBL4217716 1 6.60
CHEMBL4215077 1 6.52
CHEMBL4208409 1 6.11
CHEMBL4204035 1 6.05
CHEMBL4203405 1 6.00
CHEMBL4215740 1 5.80
CHEMBL4204319 1 5.80
CHEMBL4212766 1 5.55
CHEMBL4212788 1 -
CHEMBL4205477 1 -
CHEMBL4211795 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217195 Ki = 2.2 nM 8.66
CHEMBL4208912 Ki = 6.0 nM 8.22
CHEMBL305187 IFENPRODIL Ki = 10.0 nM 8.00
CHEMBL28564 ELIPRODIL Ki = 13.0 nM 7.89
CHEMBL4207886 Ki = 16.0 nM 7.80
CHEMBL4216511 Ki = 67.0 nM 7.17
CHEMBL4216762 Ki = 75.0 nM 7.12
CHEMBL4204069 Ki = 110.0 nM 6.96
CHEMBL4208375 Ki = 110.0 nM 6.96
CHEMBL4212243 Ki = 130.0 nM 6.89
CHEMBL4213309 Ki = 210.0 nM 6.68
CHEMBL4215178 Ki = 230.0 nM 6.64
CHEMBL4203530 Ki = 240.0 nM 6.62
CHEMBL4217716 Ki = 250.0 nM 6.60
CHEMBL4215077 Ki = 300.0 nM 6.52
CHEMBL4208409 Ki = 770.0 nM 6.11
CHEMBL4204035 Ki = 890.0 nM 6.05
CHEMBL4203405 Ki = 1000.0 nM 6.00
CHEMBL4215740 Ki = 1600.0 nM 5.80
CHEMBL4204319 Ki = 1600.0 nM 5.80
CHEMBL4212766 Ki = 2807.0 nM 5.55
CHEMBL4212788 Ki > 1000.0 nM -
CHEMBL4205477 Ki > 1000.0 nM -
CHEMBL4211795 Ki > 1000.0 nM -